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Bioorg Med Chem Lett. 2009 Oct 1;19(19):5732-6. doi: 10.1016/j.bmcl.2009.08.003. Epub 2009 Aug 6.

Identification of methysticin as a potent and non-toxic NF-kappaB inhibitor from kava, potentially responsible for kava's chemopreventive activity.

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  • 1Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard St SE, Minneapolis, MN 55455, United States.

Abstract

Nuclear factor-kappaB (NF-kappaB) is a transcription factor that plays an essential role in cancer development. The results of our recent chemopreventive study demonstrate that kava, a beverage in the South Pacific Islands, suppresses NF-kappaB activation in lung adenoma tissues, potentially a mechanism responsible for kava's chemopreventive activity. Methysticin is identified as a potent NF-kappaB inhibitor in kava with minimum toxicity. Other kava constituents, including four kavalactones of similar structures to methysticin, demonstrate minimum activities in inhibiting NF-kappaB.

PMID:
19716299
PMCID:
PMC2756981
DOI:
10.1016/j.bmcl.2009.08.003
[PubMed - indexed for MEDLINE]
Free PMC Article
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